Drug intelligence / Profile preview

digoxin + retigabine

Development stage
Unknown
Lead developer
Valeant Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Digoxin + retigabine is a combination of two pharmaceutical drugs, each with distinct mechanisms and indications. **Digoxin** is a cardiac glycoside derived from the Digitalis lanata plant, used primarily to treat heart failure and certain arrhythmias such as atrial fibrillation. It works by inhibiting the sodium-potassium ATPase pump in cardiac cells, leading to increased intracellular calcium concentrations and enhanced cardiac contractility[1][2][3][4]. **Retigabine** (also known as ezogabine) is an anticonvulsant used as adjunctive therapy for partial epilepsies in adults who have not responded adequately to other treatments. Its primary mechanism involves opening neuronal Kv7.2–Kv7.5 (KCNQ2–5) voltage-gated potassium channels, stabilizing membrane potential and reducing neuronal excitability[5][6]. Retigabine also allosterically potentiates GABA-A receptor activity[6]. The two drugs are not typically combined for a single therapeutic indication but may be co-administered in patients requiring both antiarrhythmic/cardiotonic support and seizure control; studies show no clinically relevant pharmacokinetic interaction between them[8].

Other names
digitalis glycoside (for digoxin)KCNQ channel opener (for retigabine)ezogabine (alternative name for retigabine)
02

Targets

GABRR (GABA-A receptor subunit rho)KCNQ (Potassium voltage-gated channel subfamily Q (Kv7))ABCB1 (P-glycoprotein)KCNQ5 (Potassium voltage-gated channel subfamily KQT member 5)KCNQ4 (Potassium channel subfamily KQT member 4)

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